Verapamil | Verapamil tablets 80 mg, 20 pcs.

Release form

coated tablets

Pharmacological action

Verapamil is one of the main drugs in the group of slow calcium channel blockers. It has antiarrhythmic, antianginal and antihypertensive activity.

The drug reduces myocardial oxygen demand by reducing myocardial contractility and reducing heart rate. It causes the expansion of the coronary vessels of the heart and increases coronary blood flow reduces the smooth muscle tone of peripheral arteries and the total peripheral vascular resistance.

Verapamil significantly slows atrioventricular conduction, inhibits the automatism of the sinus node, which allows the drug to be used to treat supraventricular arrhythmias.

Verapamil is the drug of choice for the treatment of angina pectoris of vasospastic origin (Prinzmetal angina pectoris). It has an effect with angina pectoris.

The action of verapamil begins 1-2 hours after ingestion, the maximum effect develops in most cases after 48 hours.

Pharmacokinetics:

When ingested, more than 90% of the dose is absorbed. Bioavailability is 10-20%. The maximum concentration of the drug in blood plasma is achieved 1-2 hours after ingestion (80-400 mg / ml). Verapamil crosses the blood-brain and placental barriers. It is metabolized during the initial passage through the liver. The main metabolites are norverapamil, N-dealkylnorverapamil. The accumulation of the drug and its metabolites in the body explains the increase in action during course treatment. Communication with plasma proteins, blood - 90%, the half-life when taking a single dose is 2.8 - 7.4 hours when taking repeated doses - 4.5 - 12 hours. It is excreted in a small amount in unchanged form (3-4%), the rest - in the form of metabolites (70%) by the kidneys, about 25% - with bile. Secretion with breast milk is low.

Indications

- Arterial hypertension.

- Coronary heart disease, including chronic stable angina pectoris (classical angina pectoris), unstable angina pectoris due to vascular spasm (Prinzmetal angina).

- Paroxysmal supraventricular tachycardia.

- Atrial fibrillation / flutter accompanied by tachyarrhythmia (with the exception of Wolff-Parkinson-White syndrome and Laun-Ganong-Levin syndrome).

Contraindications

Hypersensitivity to the drug components, severe arterial hypertension, atherosclerosis, gout, hyperuricemia, hepatitis, decompensated diabetes, peptic ulcer of the stomach and duodenum (in the acute stage), children 4 spropertosis 82 years old to the components of the drug, severe bradycardia (less than 50 beats / min), chronic heart failure at the stage of decompensation, arterial hypotension (below 100/60 mm Hg in men and 95/60 mm Hg in women), cardiogenic shock (except caused by arrhythmia), sinoatrial block, atrioventricular block II and III degree (excluding patients with an artificial pacemaker) acute myocardial infarction complicated by bradycardia, severe arterial hypotension and left ventricular failure, sinus node weakness syndrome (except for patients with an artificial pacemaker), stenosis stya aorta, Wolff-Parkinson-White syndrome, Morgagni-Adams-Stokes equations, the simultaneous use of beta-adrenobolokatorov (i.v.) syndrome Launa- Ganong-Levine, simultaneous colchicine, lactose intolerance, lactase deficiency, glucose-galactose malabsorption, pregnancy, lactation, age up to 18 years.

With caution:

With caution, administer the drug to patients with grade I atrioventricular block, severe impaired liver and kidney function, in old age, with bradycardia, hypertrophic obstructive cardiomyopathy, and diseases related to neuromuscular transmission (myasthenia gravis syndrome, , Duchenne muscular dystrophy).

Composition

Active ingredient: verapamil hydrochloride (in terms of 100% substance) - 40 mg or 80 mg

Excipients: lactose monohydrate - 26.12 mg / 52.24 mg, potato starch - 9.5 mg / 19.0 mg, talc - 0.375 mg / 0.75 mg, calcium stearate - 0.375 mg / 0.75 mg, povidone K 17 - 3.63 mg / 7.26 mg

Excipients shells: polysorbate-80 (tween-80) - 0.2 mg / 0.4 mg, titanium dioxide - 0.614 mg / 1.228 mg, hypromellose (hydroxypropyl methylcellulose) - 1.06 mg / 2.12 mg, beeswax yellow - 0.002 mg / 0.004 mg, liquid paraffin -0.12 mg / 0.24 mg, tropeolin O -0.004 mg / 0.008 mg.

Dosage and administration of

Verapamil is taken orally during or after a meal with a little water.

The dosage regimen and duration of treatment are set individually depending on the patient’s condition, severity, course of the disease and the effectiveness of therapy.

For the prevention of angina attacks, arrhythmias and in the treatment of hypertension, the drug is prescribed in an initial dose of 40-80 mg 3-4 times a day. If necessary, increase a single dose to 120-160 mg. The maximum daily dose of the drug is 480 mg.

With prolonged treatment, the daily dose of 480 mg should not be exceeded. In the maximum dose, the drug should be taken only in a hospital.

In patients with severe hepatic impairment, the removal of verapamil from the body is slow, so treatment should be started with minimal doses. The daily dose of the drug should not exceed 120 mg.

Drug interaction

When used with carbamazepine in patients with persistent partial epilepsy, verapamil enhances its effect due to inhibition of carbamazepine metabolism in the liver (risk of side effects from the central nervous system, such as diplopia, headache, ataxia and dizziness).

With the simultaneous use of verapamil inhibits the metabolism of cyclosporine in the liver, which leads to a decrease in its excretion and an increase in plasma concentration. This is accompanied by an increase in immunosuppressive action.

With the simultaneous use of verapamil increases the concentration of theophylline (due to decreased clearance).

With the simultaneous use of verapamil with quinidine, the concentration of quinidine in the blood plasma increases (the risk of a pronounced decrease in blood pressure, especially in patients with hypertrophic obstructive cardiomyopathy).

With the simultaneous use of verapamil increases the concentration of ethanol in the blood plasma and lengthens its effect.

Since verapamil inhibits the SurZa4 isoenzyme, which is involved in the metabolism of atorvastatin, lovastatin and simvastatin, drug interactions are possible due to increased plasma statins (rhabdomyolysis).

With the simultaneous use of verapamil increases the concentration in the blood plasma of almotriptan, glibenclamide.

With the simultaneous use of verapamil increases the concentration in the blood plasma of sirolimus and tacrolimus.

With the simultaneous use of verapamil increases the concentration of cardiac glycosides (requires careful monitoring and lower doses of glycosides). With the simultaneous use of verapamil increases the concentration of metoprolol and propranolol in patients with angina pectoris.

With the simultaneous use of verapamil, it increases the plasma concentration of colchicine (a substrate for the isoenzyme of surZa and p-glycoprotein).

With the simultaneous use of verapamil with doxorubicin, the concentration of doxorubicin in the blood plasma increases and its effectiveness increases.

With the simultaneous use of verapamil with imipramine, the concentration of imipramine in the blood plasma increases (the risk of developing unwanted changes, due to the additive inhibitory effect of verapamil and imipramine on AV conduction). Does not affect the concentration of the active metabolite, desipramine.

Verapamil increases the concentration of prazosin and terazosin with simultaneous use (risk of severe arterial hypotension).

With the simultaneous use of verapamil with buspirone or midazolam, their concentration in the blood plasma increases (risk of increased side effects). SurZa4 inhibitors (including erythromycin, human immunodeficiency virus protease inhibitors), telithromycin increase plasma concentrations of verapamil.

Grapefruit juice increases the concentration in the blood plasma of the r- and s-isomer of verapamil.

Cimetidine either does not change or decreases the clearance of verapamil (possibly enhancing the effects of verapamil).

Rifampicin can significantly reduce bioavailability (up to 92%), as well as the concentration of verapamil in blood plasma, which leads to a decrease in its clinical effectiveness.

Phenobarbital increases the clearance of verapamil by 5 times.

Sulfinpyrazone increases the clearance of verapamil by about 3 times and reduces bioavailability by up to 60%.

Hypericum perforatum drugs reduce the concentration of the r- and s-isomer of verapamil in blood plasma.

With the simultaneous use of verapamil with inhaled anesthetics, the risk of developing bradycardia, atrioventricular block, heart failure increases. The combination of verapamil with beta-blockers can increase the negative inotropic effect, increase the risk of developing atrioventricular conduction disturbances, bradycardia (the use of verapamil and beta-blockers must be carried out at intervals of several hours).

Prazosin and other alpha-blockers, as well as other antihypertensive drugs (angiotensin-converting enzyme inhibitors, vasodilators, diuretics, beta-blockers) enhance the antihypertensive effect of verapamil.

With the simultaneous use of verapamil with disopyramide and flecainide, severe arterial hypotension and collapse are possible, up to a fatal outcome. The risk of developing severe manifestations of drug interactions is associated with increased negative inotropic effects. Do not prescribe disopyramides and flecainide within 48 hours before or 24 hours after using verapamil, verapamil increases the risk of a neurotoxic effect of lithium preparations.

Verapamil enhances the action of peripheral muscle relaxants (may require a change in dosing regimen).

With the simultaneous use of verapamil with acetylsalicylic acid, cases of an increase in bleeding time have been described.

Overdose of

Symptoms: sinus bradycardia, passing into atrioventricular blockade of a high degree, sometimes asystole, marked decrease in blood pressure, heart failure, shock, sinus node arrest, hyperglycemia, stupor and metabolic acidosis.

Treatment for early detection - gastric lavage, activated charcoal intake, production of an artificial pacemaker for rhythm and conduction disturbances - intravenous administration of isoprenaline, norepinephrine, atropine, 10-20 ml of 10% calcium gluconate solution, artificial pacemaker, intravenous infusion of plasma-replacing solutions. Hemodialysis is not effective.

Storage conditions

In a dry, dark place and out of the reach of children at a temperature of no higher than 25 РC.

The Expiration of

is 3 years.

pharmacy leave terms

Prescription

Form of Treatment

tablets